Peringatan Keamanan

There is no information regarding the acute toxicity (LD50) and overdose of marstacimab.

Marstacimab

DB17725

biotech approved investigational

Deskripsi

Marstacimab is a human monoclonal immunoglobulin G Type 1 (IgG1) antibody produced by Chinese hamster ovary (CHO) cells by recombinant DNA technology.L51803 It is a tissue factor pathway inhibitor (TFPI) antagonist, which is an endogenous anticoagulant.A264608 Marstacimab is used to prevent bleeding episodes in patients with hemophilia,L51803 which is an X?linked bleeding disorder characterized by coagulation clotting factor deficiency.A264613 Marstacimab promotes hemostasis via the extrinsic pathway.A264613

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) In a study consisting of Chinese patients with severe hemophilia, the terminal half-life was 90.48 ± 26.025 hours following a single subcutaneous 300 mg dose.[A264598] The median time for 50% of marstacimab to be eliminated is approximately seven to 10 days.[L51803]
Volume Distribusi In patients with hemophilia, the steady-state volume of distribution was 8.6 L.[L51803]
Klirens (Clearance) In a study consisting of Chinese patients with severe hemophilia, the apparent clearance (CL/F) value was 0.06595 L/h following a single subcutaneous 300 mg dose.[A264598] Marstacimab clearance (CL) was 29% lower in adolescents (12 to <18 years of age) compared to adults (18 years and older). No clinically significant difference in adolescent marstacimab CL (L/hr/kg) compared to adults was observed after adjusting for body weight.[L51803]

Absorpsi

The bioavailability of marstacimab following subcutaneous administration is approximately 71%. In patients with hemophilia, the median Tmax ranged from 23 to 59 hours following multiple subcutaneous administrations of marstacimab.L51803 The steady-state Cmin and Cmax were calculated in adult and adolescent patients weighing at least 35 kg. Patients received a once-weekly subcutaneous dose of 150 mg. The mean Cmin (%CV) were 13.7 (90.4%) mcg/mL and 27.3 (53.2%) mcg/mL in adults and adolescents, respectively. The mean Cmax (%CV) were 17.9 (77.5%) mcg/mL and 34.7 (48.5%) mcg/mL in adults and adolescents, respectively.L51803 In a study consisting of Chinese patients with severe hemophilia, the AUCinf was 4549 ?g x h/mL following a single subcutaneous 300 mg dose.A264598

Metabolisme

Marstacimabis expected to be metabolized into small peptides and amino acids by catabolic pathways in the same manner as endogenous IgG.L51803

Rute Eliminasi

Marstacimab is cleared via linear and non-linear mechanisms. It exhibited non-linear pharmacokinetics due to target-mediated drug disposition (TMDD) which occurs when it forms marstacimab-TFPI complex. Once the target becomes saturated, the linear pathway (i.e., catabolism) dominates.L51803 Based on population pharmacokinetic analysis, about 90% of marstacimab is expected to be eliminated by the end of approximately one month after the last dose.L51803

Interaksi Obat

373 Data
Diethylstilbestrol Diethylstilbestrol may increase the thrombogenic activities of Marstacimab.
Chlorotrianisene Chlorotrianisene may increase the thrombogenic activities of Marstacimab.
Conjugated estrogens Conjugated estrogens may increase the thrombogenic activities of Marstacimab.
Estrone Estrone may increase the thrombogenic activities of Marstacimab.
Estradiol Estradiol may increase the thrombogenic activities of Marstacimab.
Dienestrol Dienestrol may increase the thrombogenic activities of Marstacimab.
Ethinylestradiol Ethinylestradiol may increase the thrombogenic activities of Marstacimab.
Mestranol Mestranol may increase the thrombogenic activities of Marstacimab.
Estriol Estriol may increase the thrombogenic activities of Marstacimab.
Estrone sulfate Estrone sulfate may increase the thrombogenic activities of Marstacimab.
Quinestrol Quinestrol may increase the thrombogenic activities of Marstacimab.
Hexestrol Hexestrol may increase the thrombogenic activities of Marstacimab.
Tibolone Tibolone may increase the thrombogenic activities of Marstacimab.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may increase the thrombogenic activities of Marstacimab.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may increase the thrombogenic activities of Marstacimab.
Polyestradiol phosphate Polyestradiol phosphate may increase the thrombogenic activities of Marstacimab.
Esterified estrogens Esterified estrogens may increase the thrombogenic activities of Marstacimab.
Zeranol Zeranol may increase the thrombogenic activities of Marstacimab.
Equol Equol may increase the thrombogenic activities of Marstacimab.
Estetrol Estetrol may increase the thrombogenic activities of Marstacimab.
Promestriene Promestriene may increase the thrombogenic activities of Marstacimab.
Methallenestril Methallenestril may increase the thrombogenic activities of Marstacimab.
Epimestrol Epimestrol may increase the thrombogenic activities of Marstacimab.
Moxestrol Moxestrol may increase the thrombogenic activities of Marstacimab.
Estradiol acetate Estradiol acetate may increase the thrombogenic activities of Marstacimab.
Estradiol benzoate Estradiol benzoate may increase the thrombogenic activities of Marstacimab.
Estradiol cypionate Estradiol cypionate may increase the thrombogenic activities of Marstacimab.
Estradiol valerate Estradiol valerate may increase the thrombogenic activities of Marstacimab.
Biochanin A Biochanin A may increase the thrombogenic activities of Marstacimab.
Formononetin Formononetin may increase the thrombogenic activities of Marstacimab.
Cetuximab The risk or severity of adverse effects can be increased when Cetuximab is combined with Marstacimab.
Human immunoglobulin G The risk or severity of adverse effects can be increased when Human immunoglobulin G is combined with Marstacimab.
Omalizumab The risk or severity of adverse effects can be increased when Omalizumab is combined with Marstacimab.
Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Marstacimab.
Abciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Marstacimab.
Gemtuzumab ozogamicin The risk or severity of adverse effects can be increased when Gemtuzumab ozogamicin is combined with Marstacimab.
Indium In-111 satumomab pendetide The risk or severity of adverse effects can be increased when Indium In-111 satumomab pendetide is combined with Marstacimab.
Infliximab The risk or severity of adverse effects can be increased when Infliximab is combined with Marstacimab.
Trastuzumab The risk or severity of adverse effects can be increased when Trastuzumab is combined with Marstacimab.
Rituximab The risk or severity of adverse effects can be increased when Rituximab is combined with Marstacimab.
Basiliximab The risk or severity of adverse effects can be increased when Basiliximab is combined with Marstacimab.
Muromonab The risk or severity of adverse effects can be increased when Muromonab is combined with Marstacimab.
Digoxin Immune Fab (Ovine) The risk or severity of adverse effects can be increased when Digoxin Immune Fab (Ovine) is combined with Marstacimab.
Ibritumomab tiuxetan The risk or severity of adverse effects can be increased when Ibritumomab tiuxetan is combined with Marstacimab.
Tositumomab The risk or severity of adverse effects can be increased when Tositumomab is combined with Marstacimab.
Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Marstacimab.
Capromab pendetide The risk or severity of adverse effects can be increased when Capromab pendetide is combined with Marstacimab.
Efalizumab The risk or severity of adverse effects can be increased when Efalizumab is combined with Marstacimab.
Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Marstacimab.
Natalizumab The risk or severity of adverse effects can be increased when Natalizumab is combined with Marstacimab.
Palivizumab The risk or severity of adverse effects can be increased when Palivizumab is combined with Marstacimab.
Daclizumab The risk or severity of adverse effects can be increased when Daclizumab is combined with Marstacimab.
Bevacizumab The risk or severity of adverse effects can be increased when Bevacizumab is combined with Marstacimab.
Technetium Tc-99m arcitumomab The risk or severity of adverse effects can be increased when Technetium Tc-99m arcitumomab is combined with Marstacimab.
Eculizumab The risk or severity of adverse effects can be increased when Eculizumab is combined with Marstacimab.
Panitumumab The risk or severity of adverse effects can be increased when Panitumumab is combined with Marstacimab.
Ranibizumab The risk or severity of adverse effects can be increased when Ranibizumab is combined with Marstacimab.
Galiximab The risk or severity of adverse effects can be increased when Galiximab is combined with Marstacimab.
Pexelizumab The risk or severity of adverse effects can be increased when Pexelizumab is combined with Marstacimab.
Afelimomab The risk or severity of adverse effects can be increased when Afelimomab is combined with Marstacimab.
Epratuzumab The risk or severity of adverse effects can be increased when Epratuzumab is combined with Marstacimab.
Bectumomab The risk or severity of adverse effects can be increased when Bectumomab is combined with Marstacimab.
Oregovomab The risk or severity of adverse effects can be increased when Oregovomab is combined with Marstacimab.
IGN311 The risk or severity of adverse effects can be increased when IGN311 is combined with Marstacimab.
Adecatumumab The risk or severity of adverse effects can be increased when Adecatumumab is combined with Marstacimab.
Labetuzumab The risk or severity of adverse effects can be increased when Labetuzumab is combined with Marstacimab.
Matuzumab The risk or severity of adverse effects can be increased when Matuzumab is combined with Marstacimab.
Fontolizumab The risk or severity of adverse effects can be increased when Fontolizumab is combined with Marstacimab.
Bavituximab The risk or severity of adverse effects can be increased when Bavituximab is combined with Marstacimab.
CR002 The risk or severity of adverse effects can be increased when CR002 is combined with Marstacimab.
Rozrolimupab The risk or severity of adverse effects can be increased when Rozrolimupab is combined with Marstacimab.
Hepatitis B immune globulin The risk or severity of adverse effects can be increased when Hepatitis B immune globulin is combined with Marstacimab.
Girentuximab The risk or severity of adverse effects can be increased when Girentuximab is combined with Marstacimab.
Obiltoxaximab The risk or severity of adverse effects can be increased when Obiltoxaximab is combined with Marstacimab.
XTL-001 The risk or severity of adverse effects can be increased when XTL-001 is combined with Marstacimab.
NAV 1800 The risk or severity of adverse effects can be increased when NAV 1800 is combined with Marstacimab.
Briakinumab The risk or severity of adverse effects can be increased when Briakinumab is combined with Marstacimab.
Otelixizumab The risk or severity of adverse effects can be increased when Otelixizumab is combined with Marstacimab.
AMG 108 The risk or severity of adverse effects can be increased when AMG 108 is combined with Marstacimab.
Iratumumab The risk or severity of adverse effects can be increased when Iratumumab is combined with Marstacimab.
Enokizumab The risk or severity of adverse effects can be increased when Enokizumab is combined with Marstacimab.
Ramucirumab The risk or severity of adverse effects can be increased when Ramucirumab is combined with Marstacimab.
Farletuzumab The risk or severity of adverse effects can be increased when Farletuzumab is combined with Marstacimab.
Veltuzumab The risk or severity of adverse effects can be increased when Veltuzumab is combined with Marstacimab.
Ustekinumab The risk or severity of adverse effects can be increased when Ustekinumab is combined with Marstacimab.
Trastuzumab emtansine The risk or severity of adverse effects can be increased when Trastuzumab emtansine is combined with Marstacimab.
PRO-542 The risk or severity of adverse effects can be increased when PRO-542 is combined with Marstacimab.
TNX-901 The risk or severity of adverse effects can be increased when TNX-901 is combined with Marstacimab.
Inotuzumab ozogamicin The risk or severity of adverse effects can be increased when Inotuzumab ozogamicin is combined with Marstacimab.
RI 624 The risk or severity of adverse effects can be increased when RI 624 is combined with Marstacimab.
Stamulumab The risk or severity of adverse effects can be increased when Stamulumab is combined with Marstacimab.
CT-011 The risk or severity of adverse effects can be increased when CT-011 is combined with Marstacimab.
Leronlimab The risk or severity of adverse effects can be increased when Leronlimab is combined with Marstacimab.
Glembatumumab vedotin The risk or severity of adverse effects can be increased when Glembatumumab vedotin is combined with Marstacimab.
Olaratumab The risk or severity of adverse effects can be increased when Olaratumab is combined with Marstacimab.
IPH 2101 The risk or severity of adverse effects can be increased when IPH 2101 is combined with Marstacimab.
TB-402 The risk or severity of adverse effects can be increased when TB-402 is combined with Marstacimab.
Caplacizumab The risk or severity of adverse effects can be increased when Caplacizumab is combined with Marstacimab.
IMC-1C11 The risk or severity of adverse effects can be increased when IMC-1C11 is combined with Marstacimab.
Eldelumab The risk or severity of adverse effects can be increased when Eldelumab is combined with Marstacimab.

Target Protein

Tissue factor pathway inhibitor TFPI

Referensi & Sumber

Artikel (PubMed)
  • PMID: 37339017
    Sun X, Liu W, Luo B, Ma D, Kalluru H, Zhou Y, Li J, Peng A, Liu Y, Tong X, Sun L, Teeter J, Raje S, Yang R: Safety, tolerability, pharmacokinetics and pharmacodynamics of a single dose of marstacimab in Chinese participants with severe haemophilia. Haemophilia. 2023 Jul;29(4):1155-1159. doi: 10.1111/hae.14814. Epub 2023 Jun 20.
  • PMID: 31336410
    Patel-Hett S, Martin EJ, Mohammed BM, Rakhe S, Sun P, Barrett JC, Nolte ME, Kuhn J, Pittman DD, Murphy JE, Brophy DF: Marstacimab, a tissue factor pathway inhibitor neutralizing antibody, improves coagulation parameters of ex vivo dosed haemophilic blood and plasmas. Haemophilia. 2019 Sep;25(5):797-806. doi: 10.1111/hae.13820. Epub 2019 Jul 23.
  • PMID: 35279938
    Mast AE, Ruf W: Regulation of coagulation by tissue factor pathway inhibitor: Implications for hemophilia therapy. J Thromb Haemost. 2022 Jun;20(6):1290-1300. doi: 10.1111/jth.15697. Epub 2022 Mar 27.
  • PMID: 36220152
    Mahlangu J, Luis Lamas J, Cristobal Morales J, Malan DR, Teeter J, Charnigo RJ, Hwang E, Arkin S: Long-term safety and efficacy of the anti-tissue factor pathway inhibitor marstacimab in participants with severe haemophilia: Phase II study results. Br J Haematol. 2023 Jan;200(2):240-248. doi: 10.1111/bjh.18495. Epub 2022 Oct 11.
  • PMID: 35316941
    Pittman DD, Rakhe S, Bowley SR, Jasuja R, Barakat A, Murphy JE: Hemostatic efficacy of marstacimab alone or in combination with bypassing agents in hemophilia plasmas and a mouse bleeding model. Res Pract Thromb Haemost. 2022 Mar 16;6(2):e12679. doi: 10.1002/rth2.12679. eCollection 2022 Feb.
  • PMID: 24620349
    Wood JP, Ellery PE, Maroney SA, Mast AE: Biology of tissue factor pathway inhibitor. Blood. 2014 May 8;123(19):2934-43. doi: 10.1182/blood-2013-11-512764. Epub 2014 Mar 11.

Contoh Produk & Brand

Produk: 1 • International brands: 0
Produk
  • Hympavzi
    Injection, solution • 150 mg/1mL • Subcutaneous • US • Approved

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